List of Compound Classes Represented in the Wiley Registry 12 Database
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Neurotransmitter Resource Guide
NEUROTRANSMITTER RESOURCE GUIDE Science + Insight doctorsdata.com Doctor’s Data, Inc. Neurotransmitter RESOURCE GUIDE Table of Contents Sample Report Sample Report ........................................................................................................................................................................... 1 Analyte Considerations Phenylethylamine (B-phenylethylamine or PEA) ................................................................................................. 1 Tyrosine .......................................................................................................................................................................................... 3 Tyramine ........................................................................................................................................................................................4 Dopamine .....................................................................................................................................................................................6 3, 4-Dihydroxyphenylacetic Acid (DOPAC) ............................................................................................................... 7 3-Methoxytyramine (3-MT) ............................................................................................................................................... 9 Norepinephrine ........................................................................................................................................................................ -
Discovery of Small Molecule and Peptide-Based Ligands for the Methyl-Lysine Binding Proteins 53Bp1 and Phf1/Phf19
DISCOVERY OF SMALL MOLECULE AND PEPTIDE-BASED LIGANDS FOR THE METHYL-LYSINE BINDING PROTEINS 53BP1 AND PHF1/PHF19 Michael Thomas Perfetti A dissertation submitted to the faculty of the University of North Carolina at Chapel Hill in partial fulfillment of the requirements for the degree of Doctor of Philosophy in the Division of Chemical Biology and Medicinal Chemistry in the Doctoral Program of the UNC Eshelman School of Pharmacy. Chapel Hill 2015 Approved by: Stephen Frye David Lawrence Albert Bowers Brian Strahl Greg Gang Wang Andrew Lee © 2015 Michael Thomas Perfetti ALL RIGHTS RESERVED ii ABSTRACT Michael Thomas Perfetti: Discovery of Small Molecule and Peptide-based Ligands for the Methyl-Lysine Binding Proteins 53BP1 and PHF1/PHF19 (Under the direction of Stephen V. Frye) Improving the understanding of the role of chromatin regulators in the initiation, development, and suppression of cancer and other devastating diseases is critical, as they are integral players in the regulation of DNA integrity and gene expression. Developing chemical tools for histone binding proteins that possess cellular activity will allow for further elucidation of the specific function of this class of histone regulating proteins. This research specifically targeted two different classes of Tudor domain containing histone binding proteins that are directly involved in the DNA damage response and modulation of gene transcription activities. The first methyl-lysine binding protein targeted was 53BP1, which is a DNA damage response protein. 53BP1 uses a tandem tudor domain (TTD) to recognize histone H4 dimethylated on lysine 20 (H4K20me2), a post-translational modification (PTM) induced by double-strand DNA breaks. -
THE BIOSYNTHESIS of SOME PHENOLIC ALKALOIDS a Thesis Submitted by GEOFFREY MELVILLE THOMAS for the Degree of DOCTOR of PHILOSOPH
/1 THE BIOSYNTHESIS OF SOME PHENOLIC ALKALOIDS a thesis submitted by GEOFFREY MELVILLE THOMAS for the degree of DOCTOR OF PHILOSOPHY of THE UNIVERSITY OF LONDON Imperial College, June 1963. London, S. W.7. ABSTRACT A brief review of the biosynthesis of alkaloids, other than those of the Amaryllidaceae and morphine groups, is given. The biosynthesis of these two groups is discussed more fully with particular reference to the evidence for the Barton and Cohen concept of phenol oxidation as a biogenetic mechanism. The incorporation of labelled phenolic precursors, derivatives of norbelladine, has been shown and by means of multiple labelled experiments incorporation as a whole, without degradation, has been proved. Other experiments described have thrown light on the earlier stages of biogenesis. The norlaudanosine derivative, (±) reticuline, has been shown to be incorporated into morphine, and an in vitro synthesis of thebaine from (±) reticuline using a radiochemical dilution method is de-scribed. I am deeply grateful to Professor D. H. R. Barton and Dr. G. W. Kirby for the privilege and pleasure of working under their supervision and for their great help in matters chemical and non-chemical. To the Salters Company I would like to express my sincere thanks for the award of a scholarship and for their interest during the tenure of it. My thanks are also due to Dr. D. W. Turner for advice on counting techniques, Mr. D. Aldrich and his staff for valuable technical assistance, Miss J. Cuckney for microanalyses, Mr. R.H. Young who grew the daffodils and poppies and to my many friends and co-workers at Imperial College. -
Pharmacology and Toxicology of Amphetamine and Related Designer Drugs
Pharmacology and Toxicology of Amphetamine and Related Designer Drugs U.S. DEPARTMENT OF HEALTH AND HUMAN SERVICES • Public Health Service • Alcohol Drug Abuse and Mental Health Administration Pharmacology and Toxicology of Amphetamine and Related Designer Drugs Editors: Khursheed Asghar, Ph.D. Division of Preclinical Research National Institute on Drug Abuse Errol De Souza, Ph.D. Addiction Research Center National Institute on Drug Abuse NIDA Research Monograph 94 1989 U.S. DEPARTMENT OF HEALTH AND HUMAN SERVICES Public Health Service Alcohol, Drug Abuse, and Mental Health Administration National Institute on Drug Abuse 5600 Fishers Lane Rockville, MD 20857 For sale by the Superintendent of Documents, U.S. Government Printing Office Washington, DC 20402 Pharmacology and Toxicology of Amphetamine and Related Designer Drugs ACKNOWLEDGMENT This monograph is based upon papers and discussion from a technical review on pharmacology and toxicology of amphetamine and related designer drugs that took place on August 2 through 4, 1988, in Bethesda, MD. The review meeting was sponsored by the Biomedical Branch, Division of Preclinical Research, and the Addiction Research Center, National Institute on Drug Abuse. COPYRIGHT STATUS The National Institute on Drug Abuse has obtained permission from the copyright holders to reproduce certain previously published material as noted in the text. Further reproduction of this copyrighted material is permitted only as part of a reprinting of the entire publication or chapter. For any other use, the copyright holder’s permission is required. All other matieral in this volume except quoted passages from copyrighted sources is in the public domain and may be used or reproduced without permission from the Institute or the authors. -
Synthesis of Isothiocyanates Using DMT/NMM/Tso− As a New Desulfurization Reagent
molecules Article Synthesis of Isothiocyanates Using DMT/NMM/TsO− as a New Desulfurization Reagent Łukasz Janczewski 1,* , Dorota Kr˛egiel 2 and Beata Kolesi ´nska 1 1 Faculty of Chemistry, Institute of Organic Chemistry, Lodz University of Technology, Zeromskiego 116, 90-924 Lodz, Poland; [email protected] 2 Department of Environmental Biotechnology, Faculty of Biotechnology and Food Sciences, Lodz University of Technology, Wolczanska 171/173, 90-924 Lodz, Poland; [email protected] * Correspondence: [email protected] Abstract: Thirty-three alkyl and aryl isothiocyanates, as well as isothiocyanate derivatives from esters of coded amino acids and from esters of unnatural amino acids (6-aminocaproic, 4-(aminomethyl)benzoic, and tranexamic acids), were synthesized with satisfactory or very good yields (25–97%). Synthesis was performed in a “one-pot”, two-step procedure, in the presence of organic base (Et3N, DBU or NMM), and carbon disulfide via dithiocarbamates, with 4-(4,6-dimethoxy-1,3,5-triazin-2-yl)-4- methylmorpholinium toluene-4-sulfonate (DMT/NMM/TsO−) as a desulfurization reagent. For the synthesis of aliphatic and aromatic isothiocyanates, reactions were carried out in a microwave reactor, and selected alkyl isothiocyanates were also synthesized in aqueous medium with high yields (72–96%). Isothiocyanate derivatives of L- and D-amino acid methyl esters were synthesized, under conditions without microwave radiation assistance, with low racemization (er 99 > 1), and their absolute configuration was confirmed by circular dichroism. Isothiocyanate derivatives of natural and unnatural amino acids were evaluated for antibacterial activity on E. coli and S. aureus bacterial strains, where the Citation: Janczewski, Ł.; Kr˛egiel,D.; most active was ITC 9e. -
The Effects of Low Dose Lysergic Acid Diethylamide Administration in a Rodent Model of Delay Discounting
Western Michigan University ScholarWorks at WMU Dissertations Graduate College 6-2020 The Effects of Low Dose Lysergic Acid Diethylamide Administration in a Rodent Model of Delay Discounting Robert J. Kohler Western Michigan University, [email protected] Follow this and additional works at: https://scholarworks.wmich.edu/dissertations Part of the Biological Psychology Commons Recommended Citation Kohler, Robert J., "The Effects of Low Dose Lysergic Acid Diethylamide Administration in a Rodent Model of Delay Discounting" (2020). Dissertations. 3565. https://scholarworks.wmich.edu/dissertations/3565 This Dissertation-Open Access is brought to you for free and open access by the Graduate College at ScholarWorks at WMU. It has been accepted for inclusion in Dissertations by an authorized administrator of ScholarWorks at WMU. For more information, please contact [email protected]. THE EFFECTS OF LOW DOSE LYSERGIC ACID DIETHYLAMIDE ADMINISTRATION IN A RODENT MODEL OF DELAY DISCOUNTING by Robert J. Kohler A dissertation submitted to the Graduate College In partial fulfillment of the requirements for the degree of Doctor of Philosophy Psychology Western Michigan University June 2020 Doctoral Committee: Lisa Baker, Ph.D., Chair Anthony DeFulio, Ph.D. Cynthia Pietras, Ph.D. John Spitsbergen, Ph.D. Copyright by Robert J. Kohler 2020 THE EFFECTS OF LOW DOSE LYSERGIC ACID DIETHYLAMIDE ADMINISTRATION IN A RODENT MODEL OF DELAY DISCOUNTING Robert J. Kohler, Ph.D. Western Michigan University, 2020 The resurgence of Lysergic Acid Diethylamide (LSD) as a therapeutic tool requires a revival in research, both basic and clinical, to bridge gaps in knowledge left from a previous generation of work. Currently, no study has been published with the intent of establishing optimal microdose concentrations of LSD in an animal model. -
Effect of Repeated MDMA Exposure on Rat Brain and Behaviour
Effect of repeated MDMA exposure on rat brain and behaviour by Ross van de Wetering A thesis submitted in fulfilment of the requirements for the degree of Doctor of Philosophy Victoria University of Wellington, New Zealand 2020 Table of contents Absract ........................................................................................................................... 5 List of abbreviations ...................................................................................................... 7 CHAPTER 1: GENERAL INTRODUCTION ............................................................ 10 Introduction ........................................................................................................................ 10 Behavioural fundamentals of addiction ........................................................................... 12 Studying addiction ........................................................................................................... 13 Self-administration. ...................................................................................................... 14 Behavioural sensitisation. ............................................................................................ 18 Neurocircuitry of addiction ............................................................................................... 20 Ventral tegmental area and nucleus accumbens .............................................................. 20 Dopamine and reinforcement. ..................................................................................... -
Mrx CLINICAL ALERT
MRx AUGUST 2018 CLINICAL ALERT YOUR MONTHLY SOURCE FOR DRUG INFORMATION HIGHLIGHTS HOT TOPIC: potential to placebo in non-dependent FIRST DRUG COMPRISED adult recreational drug users. EDITORIAL OF ACTIVE MARIJUANA DERIVATIVE APPROVED Cannabidiol oral solution was studied STAFF in 3 randomized, double-blind, placebo- Under Priority review, the United States controlled clinical trials including 516 (US) Food and Drug Administration (FDA) patients with either LGS or Dravet EDITOR IN CHIEF approved cannabidiol oral solution syndrome. Cannabidiol taken with ® Maryam Tabatabai (Epidiolex ) for the treatment of the patient’s current anticonvulsant PharmD seizures associated with Lennox-Gastaut regimen was shown to be effective syndrome (LGS) or Dravet syndrome in in reducing the frequency of seizures patients ≥ 2 years of age. It is the only when compared with placebo. Over EXECUTIVE EDITOR drug approved to treat Dravet syndrome the 12-week treatment period, the Carole Kerzic and the FDA designated it as an Orphan reduction in median number of LGS RPh drug and Rare pediatric disease drug seizures ranged from 37% to 44% with to treat both serious, difficult-to-treat CBD and 17% to 22% with placebo. DEPUTY EDITORS childhood seizure disorders. Dravet For Dravet syndrome, seizure reductions Stephanie Christofferson syndrome is diagnosed in approximately were 39% and 13% with CBD and PharmD 1 in 15,700 individuals in the US and placebo, respectively. Common side is characterized by frequent prolonged effects (≥ 10%) reported with CBD Jessica Czechowski seizures and developmental delays. LGS were increased liver transaminases PharmD involves frequent drop seizures and (particularly with concurrent use of impaired intellectual development. -
Specificity of the Antibody Receptor Site to D-Lysergamide
Proc. Nat. Acad. Sci. USA Vol. 68, No. 7, pp. 1483-1487, July 1971 Specificity of the Antibody Receptor Site to D-Lysergamide: Model of a Physiological Receptor for Lysergic Acid Diethylamide (molecular structure/hallucinogenic/rabbit/guinea pig/psychotomimetic) HELEN VAN VUNAKIS, JOHN T. FARROW, HILDA B. GJIKA, AND LAWRENCE LEVINE Graduate Department of Biochemistry, Brandeis University, Waltham, Massachusetts 02154 Commnunicated by Francis 0. Schmitt, April 21, 1971 ABSTRACT Antibodies to D-lysergic acid have been amine, and NN-dimethyl-3,4,5-trimethoxyphenylethylamine produced in rabbits and guinea pigs and a radioimmuno- were the generous gifts of Dr. W. E. Scott of Hoffmann-La assay for the hapten was developed. The specificity of this Iysergamide-antilysergamide reaction was determined by Roche. DOM (2,5-dimethoxy-4-methylamphetamine) was competitive binding with unlabeled lysergic acid diethyl- given to us by Dr. S. H. Snyder of Johns Hopkins Univer- amnide (LSD), psychotomimetic drugs, neurotransmitters, sity. Sandoz Pharmaceuticals provided us with ergonovine, and other compounds with diverse structures. LSD and methylergonovine, ergosine, and ergotomine. LSD tartarate several related ergot alkaloids were potent competitors, three to seven times more potent than lysergic acid itself. powder (Sandoz Batch no. 98601) and psilocybin powder The NN-dimethyl derivatives of several compounds, in- (Sandoz Batch no. 55001) were provided by the U.S. Food and cluding tryptamine, 5-hydroxytryptamine, 4-hydroxy- Drug Administration and the National Institute of Mental tryptamine, 5-methoxytryptamine, tyramine, and mesca- Health. line, were only about ten times less effective than lysergic Psilocin was obtained by dephosphorylating psilocybin acid, even though these compounds lack some of the ring systems of lysergic acid. -
Annex 2B Tariff Schedule of the United States See General Notes to Annex 2B for Staging Explanation HTSUS No
Annex 2B Tariff Schedule of the United States See General Notes to Annex 2B for Staging Explanation HTSUS No. Description Base Rate Staging 0101 Live horses, asses, mules and hinnies: 0101.10.00 -Purebred breeding animals Free E 0101.90 -Other: 0101.90.10 --Horses Free E 0101.90.20 --Asses 6.8% B --Mules and hinnies: 0101.90.30 ---Imported for immediate slaughter Free E 0101.90.40 ---Other 4.5% A 0102 Live bovine animals: 0102.10.00 -Purebred breeding animals Free E 0102.90 -Other: 0102.90.20 --Cows imported specially for dairy purposes Free E 0102.90.40 --Other 1 cent/kg A 0103 Live swine: 0103.10.00 -Purebred breeding animals Free E -Other: 0103.91.00 --Weighing less than 50 kg each Free E 0103.92.00 --Weighing 50 kg or more each Free E 0104 Live sheep and goats: 0104.10.00 -Sheep Free E 0104.20.00 -Goats 68 cents/head A 0105 Live poultry of the following kinds: Chickens, ducks, geese, turkeys and guineas: -Weighing not more than 185 g: 0105.11.00 --Chickens 0.9 cents each A 0105.12.00 --Turkeys 0.9 cents each A 0105.19.00 --Other 0.9 cents each A -Other: 0105.92.00 --Chickens, weighing not more than 2,000 g 2 cents/kg A 0105.93.00 --Chickens, weighing more than 2,000 g 2 cents/kg A 0105.99.00 --Other 2 cents/kg A 0106 Other live animals: -Mammals: 0106.11.00 --Primates Free E 0106.12.00 --Whales, dolphins and porpoises (mammals of the order Cetacea); manatees and dugongs (mammals of the order Sirenia) Free E 0106.19 --Other: 2B-Schedule-1 HTSUS No. -
Phenylmorpholines and Analogues Thereof Phenylmorpholine Und Analoge Davon Phenylmorpholines Et Analogues De Celles-Ci
(19) TZZ __T (11) EP 2 571 858 B1 (12) EUROPEAN PATENT SPECIFICATION (45) Date of publication and mention (51) Int Cl.: of the grant of the patent: C07D 265/30 (2006.01) A61K 31/5375 (2006.01) 20.06.2018 Bulletin 2018/25 A61P 25/24 (2006.01) A61P 25/16 (2006.01) A61P 25/18 (2006.01) (21) Application number: 11723158.9 (86) International application number: (22) Date of filing: 20.05.2011 PCT/US2011/037361 (87) International publication number: WO 2011/146850 (24.11.2011 Gazette 2011/47) (54) PHENYLMORPHOLINES AND ANALOGUES THEREOF PHENYLMORPHOLINE UND ANALOGE DAVON PHENYLMORPHOLINES ET ANALOGUES DE CELLES-CI (84) Designated Contracting States: • DECKER, Ann Marie AL AT BE BG CH CY CZ DE DK EE ES FI FR GB Durham, North Carolina 27713 (US) GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR (74) Representative: Hoeger, Stellrecht & Partner Patentanwälte mbB (30) Priority: 21.05.2010 US 347259 P Uhlandstrasse 14c 70182 Stuttgart (DE) (43) Date of publication of application: 27.03.2013 Bulletin 2013/13 (56) References cited: WO-A1-2004/052372 WO-A1-2008/026046 (73) Proprietors: WO-A1-2008/087512 DE-B- 1 135 464 • Research Triangle Institute FR-A- 1 397 563 GB-A- 883 220 Research Triangle Park, North Carolina 27709 GB-A- 899 386 US-A1- 2005 267 096 (US) • United States of America, as represented by • R.A. GLENNON ET AL.: "Beta-Oxygenated The Secretary, Department of Health and Human Analogues of the 5-HT2A Serotonin Receptor Services Agonist Bethesda, Maryland 20892-7660 (US) 1-(4-Bromo-2,5-dimethoxyphenyl)-2-aminopro pane", JOURNAL OF MEDICINAL CHEMISTRY, (72) Inventors: vol. -
Neuropharmacology and Toxicology of Novel Amphetamine-Type Stimulants
Neuropharmacology and toxicology of novel amphetamine-type stimulants Bjørnar den Hollander Institute of Biomedicine, Pharmacology University of Helsinki Academic Dissertation To be presented, with the permission of the Medical Faculty of the University of Helsinki, for public examination in lecture hall 2, Biomedicum Helsinki 1, Haartmaninkatu 8, on January 16th 2015 at 10 am. Helsinki 2015 Supervisors Thesis committee Esa R. Korpi, MD, PhD Eero Castrén, MD, PhD Institute of Biomedicine, Pharmacology Neuroscience Center Faculty of Medicine University of Helsinki P.O. Box 63 (Haartmaninkatu 8) P.O. Box 56 (Viikinkaari 4) 00014 University of Helsinki, Finland 00014 University of Helsinki, Finland Esko Kankuri, MD, PhD Sari Lauri, PhD Institute of Biomedicine, Pharmacology Neuroscience Center and Faculty of Medicine Department of Biosciences/ Physiology P.O. Box 63 (Haartmaninkatu 8) University of Helsinki 00014 University of Helsinki, Finland P.O.Box 65 (Viikinkaari 1) 00014 University of Helsinki, Finland Reviewers Dissertation opponent Atso Raasmaja, Professor, PhD Prof David Nutt DM FRCP FRCPsych Division of Pharmacology and FMedSci Pharmacotherapy Edmond J. Safra Chair of Faculty of Pharmacy Neuropsychopharmacology P. O. Box 56 (Viikinkaari 5E) Division of Brain Sciences 00014 University of Helsinki, Finland Dept of Medicine Imperial College London Petri J. Vainio, MD, PhD Burlington Danes Building Pharmacology, Drug Development and Hammersmith Hospital Therapeutics Du Cane Road Institute of Biomedicine London W12 0NN, United Kingdom Faculty of Medicine Kiinamyllynkatu 10 C 20014 University of Turku, Finland The cover layout is done by Anita Tienhaara. The cover photo is by Edd Westmacott and shows a close-up of ecstasy tablets, photographed in Amsterdam in 2004.